Entrectinib CAS 1108743-60-7 98% Purity NTRK ROS1 ALK Inhibitor Powder

High purity Entrectinib powder CAS 1108743-60-7 with 98% HPLC purity. Potent NTRK, ROS1 and ALK tyrosine kinase inhibitor for anticancer research, factory bulk supply, full certificates and fast global delivery.
Entrectinib RXDX-101 (CAS 1108743-60-7) TRK / ROS1 / ALK Inhibitor | NTRK Fusion Oncology

Entrectinib CAS 1108743-60-7
TRK / ROS1 / ALK Tyrosine Kinase Inhibitor (CNS-Active)

Entrectinib (CAS 1108743-60-7), also RXDX-101, is a potent, CNS-active inhibitor of the TRKA/B/C, ROS1 and ALK tyrosine kinases. It blocks oncogenic fusions driving NTRK-, ROS1- and ALK-rearranged tumors, inducing regression across tissue-agnostic indications (approved as Rozlytrek). Formula C31H34F2N6O2, MW 560.6. Research-grade with COA.

TRK InhibitorROS1ALKEntrectinibRXDX-101NTRK FusionOncologyCNS-Active
560.6
MW (C31H34F2N6O2)
≥98%
Purity (HPLC)
TRK/ROS1/ALK
Kinase block

Molecular Information

Name: Entrectinib (RXDX-101)
CAS: 1108743-60-7
Formula: C31H34F2N6O2
MW: 560.6 g/mol
Class: TRK/ROS1/ALK TKI
Core: Indazole benzamide piperazine
Target: TRKA/B/C, ROS1, ALK
Activity: Oncogenic-fusion blockade
MP: Not firmly reported
Appearance: White to off-white powder
Synonyms: RXDX-101
Storage: -20°C, protect from light
1108743-60-7
🧪
CAS Number
560.6
⚖️
Molecular Weight
TRK / ROS1 / ALK Inhibitor
🎯
Primary Activity
≥98%
Purity

Product Technical Specifications

Complete physicochemical properties and QC parameters for Entrectinib (CAS 1108743-60-7)

📋 Physicochemical Properties

  • Product NameEntrectinib (RXDX-101)
  • IUPAC NameN-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-2-(oxan-4-ylamino)benzamide
  • CAS Number1108743-60-7
  • SynonymsEntrectinib; RXDX-101
  • Molecular FormulaC31H34F2N6O2
  • Molecular Weight560.6 g/mol
  • SourceSynthetic kinase inhibitor
  • AppearanceWhite to off-white powder
  • Water SolubilityLow
  • Organic SolubilityDMSO; some aqueous buffers
  • Compound ClassTRK/ROS1/ALK tyrosine kinase inhibitor
  • HS Code2934.99

🔬 Quality Control & Handling

  • Purity (HPLC)≥98%
  • FormCrystalline powder
  • Primary TargetTRKA/B/C, ROS1, ALK
  • Assay ReadoutPhospho-kinase; tumor regression
  • SelectivityPan-TRK + ROS1 + ALK; CNS-penetrant
  • Storage Condition-20°C, sealed, protect from light
  • Solution StabilityDMSO stock stable weeks at -20°C
  • ShippingCold chain recommended
  • QC DocumentationCOA / HPLC / NMR / MS / MSDS
  • Pack Sizes100mg / 500mg / 1g / 5g / 10g
  • Stock StatusIn Stock
  • Use StatementResearch / investigational; not for human use

Key Molecular Targets & Pathway Nodes

Entrectinib engages the molecular machinery and pathway nodes that define its research utility.

🧬 TRKA / TRKB / TRKC (NTRK) 🧬 ROS1 🧬 ALK 🧪 MAPK / PI3K signaling 🧭 CNS tumors 🧬 Oncogenic fusions 🦴 Tumor regression 🔬 Kinase profiling 💧 Proliferation 🧭 Tissue-agnostic cancer

How Entrectinib Works: Silencing Fusion-Driven Kinases

Entrectinib blocks TRK/ROS1/ALK kinases, shutting down the signals that drive fusion-positive tumors

1

Inhibition of TRK / ROS1 / ALK Kinase Domains

Entrectinib is a small-molecule TKI that occupies the ATP-binding pockets of TRKA/B/C, ROS1 and ALK, preventing their phosphorylation and activation.

2

Suppression of Oncogenic Fusion Signaling

In NTRK-, ROS1- or ALK-rearranged cancers, these fusions constitutively drive MAPK/PI3K and proliferative signaling; entrectinib interrupts that cascade.

3

Tumor Regression & CNS Activity

Blockade halts proliferation and induces regression across tumor types regardless of tissue origin (tissue-agnostic), and its CNS penetration addresses brain metastases.

⚖️ Entrectinib vs Comparators

  • Entrectinib (this product)Pan-TRK + ROS1 + ALK; CNS-active
  • LarotrectinibSelective TRK inhibitor
  • CrizotinibROS1/ALK (less TRK) inhibitor
  • Selective EdgeBroad TRK/ROS1/ALK + brain penetration
  • Research NicheNTRK/ROS1/ALK fusion oncology

♻️ Downstream Biological Consequences

  • KinaseTRK/ROS1/ALK inhibited
  • PathwayMAPK/PI3K suppressed
  • ProliferationGrowth arrested
  • TumorRegression in fusions
  • CNSBrain metastases addressed
  • BiomarkerNTRK/ROS1/ALK testing

Research Applications & Models

Entrectinib is the reference pan-TRK/ROS1/ALK inhibitor for fusion-driven oncology.

🧭

NTRK Fusion Oncology

Benchmark pan-TRK inhibitor for tissue-agnostic NTRK-rearranged tumors.

NTRK
🧭

ROS1+ NSCLC Models

Studied in ROS1-rearranged non-small-cell lung cancer.

ROS1
🧭

ALK+ Tumors

Evaluated in ALK-positive malignancies.

ALK
🧪

Tissue-Agnostic Cancer Research

Driven by genomic alteration, not tumor site.

Tissue-agnostic
🔬

Kinase Profiling

TRK/ROS1/ALK selectivity and panel screening.

Kinase
🦴

CNS Penetration Studies

Brain-metastasis and intracranial models.

CNS

Key Literature & Landmark Publications

Landmark work on entrectinib and TRK/ROS1/ALK fusion inhibition.

Drilon A, et al. Entrectinib in ROS1+ NSCLC and NTRK fusion cancers. (clinical activity).
Landmark reference
Investigator reports. RXDX-101 TRK/ROS1/ALK inhibition.
Landmark reference
Review. Tissue-agnostic TRK inhibitors in oncology.
Landmark reference
Preclinical reports. Entrectinib CNS penetration.
Landmark reference
Structure-activity literature. Entrectinib selectivity.
Landmark reference

Available Sizes & Ordering

Research-grade Entrectinib / RXDX-101 (CAS 1108743-60-7) with full QC documentation; standard packs and bulk custom quantities supported.

TierPack SizeStock StatusSuitable ForLead Time
Standard100mgIn StockKinase / oncology assaysSame/next-day ship
Medium500mgIn StockCell & fusion studiesSame/next-day ship
Large1gIn StockIn vivo tumor modelsSame/next-day ship
Bulk5gIn StockScreening & formulationQuote to confirm
Industrial10g+Made to orderProcess developmentBatch delivery

💡 Reference sizes shown above; for exact pricing and availability please contact us for a quote. Bulk orders qualify for tiered discounts.

Frequently Asked Questions (FAQ)

What is entrectinib and what does it inhibit?
Entrectinib (CAS 1108743-60-7), also RXDX-101, is a CNS-active inhibitor of TRKA/B/C, ROS1 and ALK tyrosine kinases that block oncogenic fusions. Formula C31H34F2N6O2, MW 560.6.
Why is entrectinib called tissue-agnostic?
Its efficacy follows the presence of NTRK/ROS1/ALK rearrangements rather than tumor site, so it works across many cancer types.
Which cancers is it studied in?
NTRK-fusion solid tumors, ROS1-positive NSCLC and ALK-positive malignancies, including with CNS/brain involvement.
What readouts confirm activity?
Phospho-kinase (TRK/ROS1/ALK) suppression, downstream MAPK/PI3K signaling, proliferation/apoptosis and tumor-regression models.
How soluble is entrectinib and how should it be prepared?
It is soluble in DMSO and some aqueous buffers; poorly in water. Prepare a DMSO stock, dilute into medium (final DMSO ≤0.1% v/v), and store at -20°C protected from light.
Is QC documentation provided?
Every batch ships with a Certificate of Analysis (COA) including HPLC purity, NMR structural confirmation and MS data; MSDS/SDS and Certificates of Origin are available on request.

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Research-grade Entrectinib (CAS 1108743-60-7) — purity ≥98% HPLC, COA included
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Weight 1 g